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Kukushkin, V. Yu.; Tkachuk, V. M. published an article about the compound: cis-Dichlorobis(pyridine)platinum(II)( cas:15227-42-6,SMILESS:[Cl-][Pt+2]([N]1=CC=CC=C1)([Cl-])[N]2=CC=CC=C2 ).Formula: C10H10Cl2N2Pt. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:15227-42-6) through the article.

[Ph3PCH2Ph]2[PtXCl3] (X = Cl, NO2) are oxidized by Sb(BzCl)Cl5 (I) or Et3NCH2Ph[SbCl6] (II) in MeNO2, MeCN or DMF to give (Ph3PCH2Ph)2[PtXCl5]. SbCl5 oxidizes cis- and trans-Pt(py)2Cl2 to give cis- and trans-[Pt(py)2Cl4], resp. I oxidizes trans-[Pt(NH2CH2CO2H)2Cl2] to give trans-[Pt(NH2CH2CO2H)2Cl4] which on reaction with PCl5 in MeCN gives trans-[Pt(NH2CH2COCl)2Cl4]. [Pt(py)4]Cl2 reacted with I to give trans-[Pt(py)2Cl4]. cis- And trans-[PtL2Cl2] (L = PPh3, SMe2) are not oxidized by I or II.

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Tetrahydroisoquinoline – Wikipedia,
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Zhang, Tinghu; Kwiatkowski, Nicholas; Olson, Calla M.; Dixon-Clarke, Sarah E.; Abraham, Brian J.; Greifenberg, Ann K.; Ficarro, Scott B.; Elkins, Jonathan M.; Liang, Yanke; Hannett, Nancy M.; Manz, Theresa; Hao, Mingfeng; Bartkowiak, Bartlomiej; Greenleaf, Arno L.; Marto, Jarrod A.; Geyer, Matthias; Bullock, Alex N.; Young, Richard A.; Gray, Nathanael S. published an article about the compound: 3-(2,5-Dichloropyrimidin-4-yl)-1-(phenylsulfonyl)-1H-indole( cas:882562-40-5,SMILESS:ClC1=NC(C2=CN(C3=C2C=CC=C3)S(=O)(=O)C2=CC=CC=C2)=C(Cl)C=N1 ).SDS of cas: 882562-40-5. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:882562-40-5) through the article.

Cyclin-dependent kinases 12 and 13 (CDK12 and CDK13) play critical roles in the regulation of gene transcription. However, the absence of CDK12 and CDK13 inhibitors has hindered the ability to investigate the consequences of their inhibition in healthy cells and cancer cells. Here we describe the rational design of a first-in-class CDK12 and CDK13 covalent inhibitor, THZ531. Co-crystallization of THZ531 with CDK12-cyclin K indicates that THZ531 irreversibly targets a cysteine located outside the kinase domain. THZ531 causes a loss of gene expression with concurrent loss of elongating and hyperphosphorylated RNA polymerase II. In particular, THZ531 substantially decreases the expression of DNA damage response genes and key super-enhancer-associated transcription factor genes. Coincident with transcriptional perturbation, THZ531 dramatically induced apoptotic cell death. Small mols. capable of specifically targeting CDK12 and CDK13 may thus help identify cancer subtypes that are particularly dependent on their kinase activities.

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Hall, Matthew D.; Daly, Helen L.; Zhang, Jenny Z.; Zhang, Mei; Alderden, Rebecca A.; Pursche, Daniel; Foran, Garry J.; Hambley, Trevor W. published the article 《Quantitative measurement of the reduction of platinum(iv) complexes using X-ray absorption near-edge spectroscopy (XANES)》. Keywords: platinum complex ovarian cancer cytotoxic.They researched the compound: cis-Dichlorobis(pyridine)platinum(II)( cas:15227-42-6 ).Synthetic Route of C10H10Cl2N2Pt. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:15227-42-6) here.

The platinum(ii) drugs cisplatin, carboplatin and oxaliplatin are usefully employed against a range of malignancies, but toxicities and resistance have spurred the search for improved analogs. This has included investigation of the platinum(iv) oxidation state, which provides greater kinetic inertness. It is generally accepted that Pt(iv) complexes must be reduced to Pt(ii) for activation. As such, the ability to monitor reduction of Pt(iv) complexes is critical to guiding the design of candidates, and providing mechanistic understanding. Here we report in full that the white line height of X-ray absorption near-edge spectra (XANES) of Pt complexes, normalized to the post-edge min., can be used to quant. determine the proportion of each oxidation state in a mixture A series of Pt(iv) complexes based on the Pt(ii) complexes cisplatin and transplatin were prepared with chlorido, acetato or hydroxido axial ligands, and studies into their reduction potential and cytotoxicity against A2780 human ovarian cancer cells were performed, demonstrating the relationship between reduction potential and cytotoxicity. Anal. of white line height demonstrated a clear and consistent difference between Pt(ii) (1.52 ± 0.05) and Pt(iv) (2.43 ± 0.19) complexes. Reduction of Pt(iv) complexes over time in cell growth media and A2780 cells was observed by XANES, and shown to correspond with their reduction potentials and cytotoxicities. We propose that this method is useful for monitoring reduction of metal-based drug candidates in complex biol. systems.

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Tetrahydroisoquinoline – Wikipedia,
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Quality Control of cis-Dichlorobis(pyridine)platinum(II). Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: cis-Dichlorobis(pyridine)platinum(II), is researched, Molecular C10H10Cl2N2Pt, CAS is 15227-42-6, about Chemical assembling of silica surface using a reaction of catalytic hydrosilylation. Author is Vekki, D. A.; Kuchaev, E. A..

Chem. assembling of the silica surface modified by dimethylchlorosilane was performed by the catalytic hydrosilylation of 1,3-divinyl-1,1,3,3-tetramethyldisiloxane, α-Me styrene, acetophenone, allyl Bu and allyl glycidyl ethers with dimethylchlorosilane. The effect of the nature of complexes of platinum, palladium, rhodium and ruthenium on the parameters of hydrosilylation was studied. It was shown that the maximum rate of hydrosilylation was observed in the reaction with allyl glycidyl ether, and min., with α-methylstyrene; the most effective catalyst of hydrosilylation was [Rh(CO)2(acac)].

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Tetrahydroisoquinoline – Wikipedia,
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HPLC of Formula: 15227-42-6. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: cis-Dichlorobis(pyridine)platinum(II), is researched, Molecular C10H10Cl2N2Pt, CAS is 15227-42-6, about The investigation of platinum(II) complexes with adenine, adenosine and 2-aminopyrimidines. Author is Stetsenko, A. I.; Dmitrieva, E. S.; Yakovlev, K. I..

[Pt2(NH3)4Cl2L]Cl2 (L = adenine, adenosine) were prepared by the addition of ligand to cis-[Pt(NH3)2Cl2] solution [Pt(NH3)2L](NO3)2 were obtained by adding L to cis-[Pt(NH3)2(H2O)2](NO3)2 solution 2-Aminopyrimidine (L1) and 2-amino-4-phenylpyrimidine (L2) reacted with aqueous K2[PtCl4] to yield trans-[PtL12Cl2] and trans-[PtL22Cl2], resp. The cis-[PtA2L12]Cl2 (A = NH3, pyridine, 0.5 ethylenediamine) were obtained by the substitution reaction of cis-[PtA2Cl2] with 2-aminopyrimidine. The cis-[PtA2(H2O)2](NO3)2 reacted with 2-aminopyrimidine to afford cis-[PtA2L12](NO3)2 and cis-[PtA2L1](NO3)2 (A = NH3, 0.5 ethylenediamine), depending on the stoichiometric ratios of the reactants.

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Tetrahydroisoquinoline – Wikipedia,
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Synthetic Route of C10H10Cl2N2Pt. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: cis-Dichlorobis(pyridine)platinum(II), is researched, Molecular C10H10Cl2N2Pt, CAS is 15227-42-6, about Bis(pentafluorophenyl) complexes of palladium(II) and of platinum(II). Author is Uson, R.; Fornies, J.; Gimeno, J.; Espinet, P.; Navarro, R..

The preparation of 8 bis(pentafluorophenyl) complexes of Pd(II) and of Pt(II) with monodentate and bidentate N-donor ligands is described together with a preparation of a Pd(II) complex of 1,2-bis(diphenylphosphino)ethane. Assignments of cis or trans configuration are discussed which depend upon the splitting or disappearance of certain bands in ir.

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Kukushkin, Yu. N.; Sedova, G. N.; Belyaev, A. N.; Konovalov, L. V. published an article about the compound: cis-Dichlorobis(pyridine)platinum(II)( cas:15227-42-6,SMILESS:[Cl-][Pt+2]([N]1=CC=CC=C1)([Cl-])[N]2=CC=CC=C2 ).Formula: C10H10Cl2N2Pt. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:15227-42-6) through the article.

The thermal behavior of onium chloroplatinates of the type (AH)2[PtCl6] (A = NH3, MeNH2, 0.5 en, piperidine, py, γ-picoline, NH2Ph, p-toluidine, quinoline, 0.5 2,2′-bipyridine) was studied by derivatog. and IR spectral anal. The heating of solid (AH)2[PtCl6] led to the formation of trans-PtL2Cl4 (L = py, γ-picoline) and cis-PtQ2Cl4 (Q = p-toluidine) and subsequently to the formation of cis-PtA2Cl2. When (AH)2[PtCl6] (A = piperidine) was heated (AH)2[PtCl4] was formed. These results were compared with those for the corresponding palladates.

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Tetrahydroisoquinoline – Wikipedia,
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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: cis-Dichlorobis(pyridine)platinum(II), is researched, Molecular C10H10Cl2N2Pt, CAS is 15227-42-6, about Activation of the trans geometry in platinum antitumor complexes. Synthesis, characterization, and biological activity of complexes with the planar ligands pyridine, N-methylimidazole, thiazole, and quinoline. Crystal and molecular structure of trans-dichlorobis(thiazole)platinum(II), the main research direction is antitumor platinum chloro nitrogen donor complex; crystal structure platinum chloro thiazole complex.Reference of cis-Dichlorobis(pyridine)platinum(II).

The presence of planar ligands in trans-[PtCl2(py)2] greatly enhances the cytotoxicity of such species, with respect both to their corresponding cis isomer and also to trans-[PtCl2(NH3)2]. The cytotoxicity of trans-[PtCl2(py)2] in murine tumor cell lines is equivalent to the anticancer drug cisplatin, cis-[PtCl2(NH3)2]. The generality of this effect was studied for a range of structures with planar ligands of formula trans-[PtCl2(L)(L’)]. Three distinct series were examined-(1) L = L’ = py, N-methylimidazole (N-MeIm), and thiazole (Tz), (2) L = quinoline (quin), L’ = MeRSO where (R = Me, CH2Ph, Ph), and (3) L = quinoline, L’ = NH3. The synthesis and chem. characterization of all new complexes are described. An x-ray crystal structure determination for trans-[PtCl2(Tz)2] confirmed the geometry with N-bound thiazole. The crystals are monoclinic, space group C2/c, a 8.088(3), b 14.964(4), c 8.847(2) Å, β 99.50(2), Z = 4, R = 0.0545, Rw = 0.0655. Pt has the expected square planar coordination with l(Pt-Cl) = 2.300(5) Å and l(Pt-N) = 2.024(18) and 2.077(17) Å. Bond angles are normal with N(1)-Pt-N(2) = 180.0(1)°, N(1)-Pt-Cl(1) = 90.4(1)°, and N(2)-Pt-Cl(1A) = 89.6(1)°. The intensity data were collected with MoKα radiation with λ = 0.71073 Å. The thiazole rings are not coplanar but slightly tilted to each other at an angle of 14.3°. The dihedral angles between the Pt coordination plane and the thiazole rings are 119.3 and 105.0°. The biol. studies confirm the generality of activation of the trans geometry using planar ligands. Cytotoxicity tests in murine leukemia (L1210) cell lines both sensitive and rendered resistant to cisplatin show that the complexes show equivalent cytostatic activity to that of cisplatin. The activity is an order of magnitude greater than trans-[PtCl2(NH3)2]. The cytotoxicity is further marked by consistent activity in the cisplatin-resistant cell line. Contrary to the well-established but empirical structure-activity relationships, the trans geometry can give platinum complexes with cytotoxicity equivalent to that of the analogous cis isomer. The results point to a further source of platinum antitumor complexes acting by a different mol. mechanism to cisplatin with potential for antitumor activity complementary to that of the clin. used drug.

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Tetrahydroisoquinoline – Wikipedia,
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Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 15227-42-6, is researched, SMILESS is [Cl-][Pt+2]([N]1=CC=CC=C1)([Cl-])[N]2=CC=CC=C2, Molecular C10H10Cl2N2PtJournal, Article, Chemico-Biological Interactions called Interactions of an antitumor platinum compound with deoxyribonucleic acid, histones, L-amino acids, poly(L-amino acids), nucleosides, and nucleotides, Author is Morris, Carl R.; Gale, Glen R., the main research direction is neoplasm inhibitor platinum compound; DNA platinum compound; amino acid platinum compound; protein platinum compound; nucleic acid component platinum compound.Application In Synthesis of cis-Dichlorobis(pyridine)platinum(II).

The antitumor agents cis-dichloro(dipyridine)platinum(II) [15227-42-6] and cis-dichlorodiammineplatinum(II) [15663-27-1] interacted not only with DNA but also with amino acids, histones, polyamino acids, nucleosides, and nucleotides. The platinum complexes apparently associated with electron-rich areas of the various components. Such interactions could significantly affect pool levels of these cell components, cellular metabolism, and the pharmacol. action of the platinum compounds

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So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Lange, Andreas; Guenther, Marcel; Buettner, Felix Michael; Zimmermann, Markus O.; Heidrich, Johannes; Hennig, Susanne; Zahn, Stefan; Schall, Christoph; Sievers-Engler, Adrian; Ansideri, Francesco; Koch, Pierre; Laemmerhofer, Michael; Stehle, Thilo; Laufer, Stefan A.; Boeckler, Frank M. researched the compound: 3-(2,5-Dichloropyrimidin-4-yl)-1-(phenylsulfonyl)-1H-indole( cas:882562-40-5 ).SDS of cas: 882562-40-5.They published the article 《Targeting the Gatekeeper MET146 of C-Jun N-Terminal Kinase 3 Induces a Bivalent Halogen/Chalcogen Bond》 about this compound( cas:882562-40-5 ) in Journal of the American Chemical Society. Keywords: aminopyrimidine inhibitor halogen chalcogen bond methionine JNK3 crystal structure. We’ll tell you more about this compound (cas:882562-40-5).

We target the gatekeeper MET146 of c-Jun N-terminal kinase 3 (JNK3) to exemplify the applicability of X···S halogen bonds in mol. design using computational, synthetic, structural and biophys. techniques. In a designed series of aminopyrimidine-based inhibitors, we unexpectedly encounter a plateau of affinity. Compared to their QM-calculated interaction energies, particularly bromine and iodine fail to reach the full potential according to the size of their σ-hole. Instead, mutation of the gatekeeper residue into leucine, alanine, or threonine reveals that the heavier halides can significantly influence selectivity in the human kinome. Thus, we demonstrate that, although the choice of halogen may not always increase affinity, it can still be relevant for inducing selectivity. Determining the crystal structure of the iodine derivative in complex with JNK3 (4X21) reveals an unusual bivalent halogen/chalcogen bond donated by the ligand and the back-pocket residue MET115. Incipient repulsion from the too short halogen bond increases the flexibility of Cε of MET146, whereas the rest of the residue fails to adapt being fixed by the chalcogen bond. This effect can be useful to induce selectivity, as the necessary combination of methionine residues only occurs in 9.3% of human kinases, while methionine is the predominant gatekeeper (39%).

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Tetrahydroisoquinoline – Wikipedia,
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